- An efficient process for the large-scale synthesis of a 2,3,6-trisubstituted indole
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The efficient synthesis of a key trisubstituted indole intermediate 1 is described. The synthetic route required the use of an aryl Grignard reagent which was not commercially available, and the large-scale formation of this fragment and the thermal evalu
- Alorati, Anthony D.,Gibb, Andrew D.,Mullens, Peter R.,Stewart, Gavin W.
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p. 1947 - 1952
(2013/03/14)
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- Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
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Herein, we present initial SAR studies on a series of bridged 2-arylindole-based NS5B inhibitors. The introduction of bridging elements between the indole N1 and the ortho-position of the 2-aryl moiety resulted in conformationally constrained heterocycles
- Zheng, Xiaofan,Hudyma, Thomas W.,Martin, Scott W.,Bergstrom, Carl,Ding, Min,He, Feng,Romine, Jeffrey,Poss, Michael A.,Kadow, John F.,Chang, Chong-Hwan,Wan, John,Witmer, Mark R.,Morin, Paul,Camac, Daniel M.,Sheriff, Steven,Beno, Brett R.,Rigat, Karen L.,Wang, Ying-Kai,Fridell, Robert,Lemm, Julie,Qiu, Dike,Liu, Mengping,Voss, Stacey,Pelosi, Lenore,Roberts, Susan B.,Gao, Min,Knipe, Jay,Gentles, Robert G.
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scheme or table
p. 2925 - 2929
(2011/06/26)
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- Discovery of (7 R)-14-Cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6 H -indolo[1,2- e ][1,5]benzoxazocine-11-carboxylic Acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase
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Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. The polymerase of HCV is responsible for the replication of viral genome and has been a prime target for drug discovery eff
- Narjes, Frank,Crescenzi, Benedetta,Ferrara, Marco,Habermann, J?rg,Colarusso, Stefania,Del Rosario Rico Ferreira, Maria,Stansfield, Ian,MacKay, Angela Claire,Conte, Immacolata,Ercolani, Caterina,Zaramella, Simone,Palumbi, Maria-Cecilia,Meuleman, Philip,Leroux-Roels, Geert,Giuliano, Claudio,Fiore, Fabrizio,Di Marco, Stefania,Baiocco, Paola,Koch, Uwe,Migliaccio, Giovanni,Altamura, Sergio,Laufer, Ralph,De Francesco, Raffaele,Rowley, Michael
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supporting information; experimental part
p. 289 - 301
(2011/03/22)
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- PENTACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to pentacyclic indole derivatives of formula (I): wherein A, Ar, R1, R2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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Page/Page column 27
(2008/06/13)
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- Inhibitors of HCV replication
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Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
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Page/Page column 25; 43-44
(2010/10/20)
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- Discovery of conformationally constrained tetracyclic compounds as potent hepatitis C virus NS5B RNA polymerase inhibitors
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We report a new series of hepatitis C virus NS5B RNA polymerase inhibitors containing a conformationally constrained tetracyclic scaffold. SAR studies led to the identification of 6,7-dihydro-5H-benzo[5,6][1,4]diazepino[7,1-a]indoles (19 and 20) bearing a basic pendent group with high biochemical and cellular potencies. These compounds displayed a very small shift in cellular potency when the replicon assay was performed in the presence of human serum albumin.
- Ikegashira, Kazutaka,Oka, Takahiro,Hirashima, Shintaro,Noji, Satoru,Yamanaka, Hiroshi,Hara, Yoshinori,Adachi, Tsuyoshi,Tsuruha, Jun-Ichiro,Doi, Satoki,Hase, Yasunori,Noguchi, Toru,Ando, Izuru,Ogura, Naoki,Ikeda, Satoru,Hashimoto, Hiromasa
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p. 6950 - 6953
(2007/10/03)
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- TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, A, Ar, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
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Page/Page column 30
(2010/11/08)
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